Eulexin: Advanced Androgen Blockade for Prostate Cancer Control
| Product dosage: 250mg | |||
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Synonyms
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Eulexin (flutamide) is a nonsteroidal antiandrogen agent indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) agonist for the management of metastatic prostate carcinoma. It competitively inhibits androgen uptake and nuclear binding in target tissues, providing a critical component in combined androgen blockade strategies. This oral medication is specifically formulated to interfere with testosterone activity at the cellular level, helping to control disease progression and manage symptoms in appropriate patient populations.
Features
- Nonsteroidal antiandrogen with specific competitive binding activity
- Oral administration with 250 mg scored tablets
- Bioavailability of approximately 90-95% following oral ingestion
- Extensive hepatic metabolism with multiple active metabolites
- Plasma protein binding exceeding 94-96%
- Elimination half-life of approximately 5-6 hours for parent compound
Benefits
- Effectively reduces androgen stimulation of prostate cancer cells when combined with LHRH therapy
- Helps delay disease progression in metastatic prostate carcinoma
- Contributes to reduction in tumor-related symptoms and PSA levels
- Provides oral dosing convenience for long-term management
- Works synergistically with medical castration approaches
- Offers targeted antiandrogen activity with well-characterized pharmacokinetics
Common use
Eulexin is primarily prescribed as combination therapy with LHRH agonists (such as leuprolide or goserelin) for the treatment of metastatic prostate cancer. This combination approach achieves complete androgen blockade by simultaneously suppressing testicular androgen production (via LHRH agonist) and blocking androgen receptor binding in peripheral tissues (via flutamide). The medication is typically initiated concurrently with LHRH therapy and continued throughout treatment duration unless contraindicated by adverse effects or disease progression.
Dosage and direction
The recommended adult dosage is one 250 mg tablet administered orally three times daily at approximately 8-hour intervals. Administration with food is acceptable as it does not significantly affect bioavailability. Tablets should be swallowed whole with water, though they may be divided along the score line if dose adjustment is necessary. Treatment should continue as long as clinical benefit is observed, typically until disease progression or unacceptable toxicity occurs. Dosage modification may be required in patients with hepatic impairment.
Precautions
Regular monitoring of liver function tests is essential, particularly during the first four months of therapy. Patients should be advised regarding potential hepatotoxicity and instructed to report symptoms such as nausea, vomiting, abdominal pain, fatigue, dark urine, or jaundice promptly. Periodic measurement of prostate-specific antigen (PSA) levels helps monitor treatment response. Blood counts should be monitored regularly due to potential hematological effects. Patients with glucose-6-phosphate dehydrogenase deficiency should be monitored for hemolytic anemia. Caution is advised in patients with pre-existing hepatic conditions.
Contraindications
Eulexin is contraindicated in patients with known hypersensitivity to flutamide or any component of the formulation. It should not be used in patients with severe hepatic impairment (Child-Pugh Class C). The medication is contraindicated in women, particularly during pregnancy, due to potential fetal harm. It must not be administered to pediatric patients. Concurrent use with certain medications that prolong QT interval requires careful risk-benefit assessment.
Possible side effects
Common adverse reactions include hot flashes (50-60% of patients), loss of libido (30-40%), diarrhea (10-15%), nausea and vomiting (5-10%), and gynecomastia (30-50%). Less frequent but potentially serious effects include hepatotoxicity (2-4%, ranging from transaminase elevations to fatal hepatic necrosis), hematological abnormalities (anemia, leukopenia, thrombocytopenia), and cardiovascular effects. Other reported side effects include visual disturbances, peripheral edema, hypertension, and rash. Most adverse effects are dose-dependent and may require symptomatic management or dosage adjustment.
Drug interaction
Eulexin may interact with warfarin and other coumarin derivatives, potentially increasing anticoagulant effect and requiring close monitoring of prothrombin time. Concurrent use with medications that induce hepatic enzymes (phenytoin, rifampin, carbamazepine) may reduce flutamide concentrations. Drugs that inhibit CYP1A2 (such as fluvoxamine) may increase flutamide exposure. Caution is advised with other hepatotoxic medications due to additive liver injury risk. The medication may alter glucose tolerance, potentially requiring adjustment of antidiabetic regimens.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistent dosing intervals are important for maintaining stable drug concentrations and optimal androgen blockade. Healthcare providers should be consulted if multiple doses are missed or if questions arise regarding dosing schedule.
Overdose
There is limited experience with Eulexin overdose. Symptoms may include exaggerated pharmacological effects such as nausea, vomiting, dizziness, and potential hepatic toxicity. In case of suspected overdose, gastric lavage or activated charcoal administration may be considered if presentation is prompt. Supportive care should be provided with particular attention to hepatic function monitoring. No specific antidote exists, and treatment should focus on symptomatic management and supportive measures. Dialysis is unlikely to be effective due to high protein binding.
Storage
Store at controlled room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). Keep container tightly closed and protect from moisture and light. Tablets should be kept in their original packaging until administration. Keep out of reach of children and pets. Do not use beyond the expiration date printed on packaging. Proper disposal of unused medication should follow local regulations for pharmaceutical waste.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient circumstances. The prescribing physician should be consulted for complete information regarding indications, dosage, administration, and monitoring requirements. Patients should not alter or discontinue medication without medical supervision.
Reviews
Clinical studies demonstrate that Eulexin in combination with LHRH agonists provides superior objective response rates and progression-free survival compared to monotherapy in metastatic prostate cancer. The combination approach shows significant advantages in time to treatment failure and overall survival in appropriate patient populations. Most clinical trials report acceptable tolerability profiles with manageable side effects when properly monitored. Long-term follow-up data support the sustained efficacy of combined androgen blockade in metastatic disease management.